中文名稱:庫潘尼西 | 英文名稱:Copanlisib |
CAS:1032568-63-0 | 品牌: TargetMol |
產(chǎn)地: 美國 | 保存條件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
純度規(guī)格: 99.88% | 產(chǎn)品類別: 抑制劑 |
貨號: T6322 |
名稱 | Copanlisib |
描述 | Copanlisib (BAY 80-6946) is a phosphoinositide 3-kinase (PI3K) inhibitor with potential antineoplastic activity. Copanlisib inhibits the activation of the PI3K signaling pathway, which may result in inhibition of tumor cell growth and survival in susceptible tumor cell populations. Activation of the PI3K signaling pathway is frequently associated with tumorigenesis and dysregulated PI3K signaling may contribute to tumor resistance to a variety of antineoplastic agents. |
細(xì)胞實(shí)驗(yàn) | Cell proliferation over a 72-hour period is determined using the CellTiter-Glo? luminescent cell viability kit. Briefly, cells are plated in separate microtiter plates. Following an overnight incubation at 37oC, luminescence values in the t=0 hour plates are determined. Test compounds diluted in growth medium are added to the t=72 hour plates, and the cells are then incubated for 72 hours at 37oC. Luminescence values are determined with a Wallac 1420 Victor2? 1420 multilabel HTS counter after a 10-minute reaction with CellTiter-Glo? solution. The percentage inhibition of cell growth is calculated by subtracting the luminescence values in the t=0 hour plates from the corresponding values in the t=72 hour plates. Differences in values between drug-treated cells and controls are used to determine the percentage inhibition of cell growth.(Only for Reference) |
激酶實(shí)驗(yàn) | Biochemical lipid kinase assays: The effect of BAY 80-6946 on PI3Kα, PI3Kβ, and PI3Kγ activity is measured by the inhibition of 33P incorporation into phosphatidylinositol (PI) in 384-well MaxiSorp? plates coated with 2 μg/well of PI and phosphatidylserine (PS) (1:1 molar ratio). In each PI3K isoform assay, 9 μL of reaction buffer (50 mM MOPSO, pH 7.0, 100 mM NaCl, 4 mM MgCl2, 0.1% BSA) containing 7.5 ng of His-tagged N-terminal truncated p110α or p110β protein, or 25 ng of purified human p110γ protein, is used. The reaction is started by adding 5 μL of a 40-μM ATP solution containing 20 μCi/mL [33>/sup>P]-ATP. After 2 hours incubation at room temperature, the reaction is terminated by addition of 5 μL of a 25-mM EDTA solution. The plates are washed and Ultima Gold? scintillation cocktail (25 μL) is then added. The radioactivity incorporated into the immobilized PI substrate is determined with a BetaPlate Liquid Scintillation Counter. |
體外活性 | 在KPL4細(xì)胞和LPA刺激的PC3細(xì)胞中,Copanlisib降低pAKT水平。在一組存在PIK3CA突變和/或HER2過表達(dá)的人類癌癥細(xì)胞系中,Copanlisib展示了抗增殖活性并誘導(dǎo)了凋亡。[1] HER2靶向療法與Copanlisib的聯(lián)合應(yīng)用比單獨(dú)使用任一療法更有效地抑制增長,并能在細(xì)胞中恢復(fù)對trastuzumab和lapatinib的敏感性。[2] |
體內(nèi)活性 | 在大鼠KPL4或HCT116腫瘤異種移植模型中,Copanlisib(6 mg/kg,靜脈注射)可誘導(dǎo)100%的完全腫瘤消退。在攜帶Lu7860厄洛替尼耐藥、源自患者的非小細(xì)胞肺癌和MAXF1398源自患者的腺泡狀乳腺腫瘤模型的裸鼠中,Copanlisib(14 mg/kg,靜脈注射)同樣可抑制腫瘤生長。[1] |
存儲條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度 | DMSO : < 1 mg/mL (insoluble or slightly soluble) H2O : Insoluble 0.01M HCl : 10 mg/mL (20.81 mM), Sonication is recommended. |
關(guān)鍵字 | PI3K | Apoptosis | antiproliferative | antitumor | Inhibitor | administration | phosphorylation | sub-nanomolar | AKT | Phosphoinositide 3-kinase | inhibit | Copanlisib | intravenous |
相關(guān)產(chǎn)品 | L-Glutamic acid | Metronidazole | 5-Fluorouracil | Dextran sulfate sodium salt (MW 4500-5500) | Stavudine | Tributyrin | Myricetin | Sorafenib | L-Ascorbic acid | Acetylcysteine | Salicylic acid | Sodium 4-phenylbutyrate |
相關(guān)庫 | 抗癌上市藥物庫 | 經(jīng)典已知活性庫 | 抗癌活性化合物庫 | 抗衰老化合物庫 | FDA 上市藥物庫 | 藥物功能重定位化合物庫 | 抗癌藥物庫 |
成立日期 | 2013-04-18 (12年) | 注冊資本 | 566.2651萬人民幣 |
員工人數(shù) | 100-500人 | 年?duì)I業(yè)額 | ¥ 1億以上 |
主營行業(yè) | 化學(xué)試劑,生物活性小分子 | 經(jīng)營模式 | 貿(mào)易,試劑,定制,服務(wù) |
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